Singh Priya, Adhikari Anupriya, Singh Deepika, Gond Chandraprakash, Tiwari Anjani Kumar
Department of Chemistry, Babasaheb Bhimrao Ambedkar University (A Central University), Lucknow, 226025, Uttar Pradesh, India.
ACS Omega. 2022 Apr 18;7(17):14412-14429. doi: 10.1021/acsomega.2c00588. eCollection 2022 May 3.
Translocator protein (TSPO, 18 kDa) is an evolutionary, well-preserved, and tryptophan-rich 169-amino-acid protein which localizes on the contact sites between the outer and inner mitochondrial membranes of steroid-synthesizing cells. This mitochondrial protein is implicated in an extensive range of cellular activities, including steroid synthesis, cholesterol transport, apoptosis, mitochondrial respiration, and cell proliferation. The upregulation of TSPO is well documented in diverse disease conditions including neuroinflammation, cancer, brain injury, and inflammation in peripheral organs. On the basis of these outcomes, TSPO has been assumed to be a fascinating subcellular target for early stage imaging of the diseased state and for therapeutic purposes. The main outline of this Review is to give an update on dealing with the advances made in TSPO PET tracers for neuroinflammation, synchronously emphasizing the approaches applied for the design and advancement of new tracers with reference to their structure-activity relationship (SAR).
转位蛋白（TSPO，18 kDa）是一种经过进化且保存完好的富含色氨酸的169个氨基酸的蛋白质，定位于类固醇合成细胞线粒体外膜与内膜的接触部位。这种线粒体蛋白参与广泛的细胞活动，包括类固醇合成、胆固醇转运、细胞凋亡、线粒体呼吸和细胞增殖。TSPO的上调在多种疾病状态下都有充分记录，包括神经炎症、癌症、脑损伤和外周器官炎症。基于这些结果，TSPO被认为是疾病状态早期成像和治疗目的的一个极具吸引力的亚细胞靶点。本综述的主要内容是更新TSPO正电子发射断层显像（PET）示踪剂在神经炎症方面的进展，同时参照其构效关系（SAR）强调用于设计和改进新型示踪剂的方法。
